LECTURE 7 Flashcards

1
Q

MORPHINE

A

ALLOWS FOR DOSE-RELATED ANALGESIA AND **INCREASED PAIN TOLERANCE
CAN CAUSE EUPHORIA; HOWEVER, IF ADMINISTERED TO A PERSON WHO IS PAIN FREE, IT CAN CAUSE DYSPHORIA, ANXIETY, MENTAL CLOUDING
SIDE EFFECTS - RESPIRATORY DEPRESSANT, COUGH SUPPRESSANT

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2
Q

MORPHINE BIPHASIC DOSE-DEPENDENT EFFECT ON BODY TEMPERATURE

A

LOW DOSE - CAUSES A DECREASE IN BODY TEMPERATURE

HIGH DOSE - CAUSES AN INCREASE IN BODY TEMPERATURE

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3
Q

HYDROMORPHONE

A

(DILAUDID)
ORAL ADMINISTRATION (15-30 MIN)
IV ADMINISTRATION (5 MIN)
RAPIDLY ABSORBED, HIGH 1ST PASS METABOLISM
**3-5X MORE POTENT WHEN GIVEN ORALLY AS MORPHINE (NO INACTIVE/ACTIVE METABOLITES - NO NEED TO WORRY ABOUT PATIENT TO PATIENT VARIABILITIES)
USED FOR MILD TO STRONG PAIN IN HOSPITALS
PHARMACOKINETICS SIMILAR TO MORPHINE

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4
Q

FENTANYL

A

MANY DIFFERENT WAYS OF ADMINISTERING
ORAL, BUCCAL (5-15 min.), IM (7-8 min.), NASAL SPRAY, IV (immediate), TRANSDERMAL (6h), LOLLIPOPS, LOZENGES
HIGHLY LIPOPHILIC - GETS THROUGH MEMBRANES QUICKLY
80x ANALGESIC POTENCY OF MORPHINE, 10x ANALGESIC POTENCY OF HYDROMORPHONE
**USED FOR BREAKTHROUGH PAIN IN COMBINATION W/ ANOTHER OPIOID FOR CHRONIC PAIN
**HIGH ABUSE POTENTIAL
**SHORT TERM RELIEF

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5
Q

INTERMEDIATE OPIOIDS

A

**OXYCODONE - SIMILAR EFFICACY TO MORPHINE BUT HAS BETTER ORAL BIOAVAILABILITY (THEBAINE DERIVATIVE)
METHADONE - HIGH POTENCY, LONG DURATION OF ACTION, GOOD ORAL BIOAVAILABILITY, A LOT OF INTER-PATIENT VARIABILITY
**USED FOR OPIOID ADDICTION
BUPRENORPHINE - SL/TD ADMINISTRATION, MU OPIOID EFFICACY AGONIST AND HAS KAPPA ANTAGONIST ABILITIES (GOOD FOR ANALGESIA AND OPIOID ADDICTIONS)

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6
Q

WEAK OPIOIDS

A

TRAMADOL - WEAK MU AGONIST W/ 5-HT AND NOREPINEPHRINE REUPTAKE INHIBITION (GOOD ORAL BIOAVAILABILITY)
**COMBINES ANTIDEPRESSANT REACTIONS W/ OPIOID REACTIONS
TAPENTADOL - MU AGONIST W/ NE REUPTAKE INHIBITION (B/C NO SEROTONIN REUPTAKE INHIBITION AND STRONG NE REUPTAKE INHIBITION W/ SAME MECHANISM AS COCAINE AND AMPHETAMINE => **HIGH POTENTIAL FOR ABUSE)

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7
Q

CODEINE METABOLISM

A

CATALYZED TO MORPHINE BY CYP2D6 ENZYME
POLYMORPHISMS IN CYP2D6 =>
1.) INABILITY TO CONVERT CODEINE TO MORPHINE IN 10% OF CAUCASIANS
2.) ULTRA-RAPID CATALYSIS OF CODEINE TO MORPHINE AND AN INCREASE IN SENSITIVITY IN 4-5% OF US POPULATION AND 16-28% OF NORTH AFRICANS, ETHIOPIANS, AND ARABS

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8
Q

NALOXONE (NARCANE)

A

OPIATE ANTAGONIST - REVERSES RESPIRATORY EFFECTS OF OPIOID AGONISTS
PHARMACOKINETICS =
IM, SUBQ = 2-5 MIN., INHALATION ~5 MIN., INTRANASAL 8-13 MIN., IV ~2 MIN.
DURATION OF ACTION = 30-120 MIN. (REPEATED DOSES ARE USUALLY NEEDED)
REVERSES ALL EFFECTS OF OPIOID AGONISTS AND BLOCKS MU, KAPPA, AND DELTA RECEPTORS

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9
Q

ARACHIDONIC ACID

A

EICOSANOID PRECURSOR - RELEASED FROM PHOSPHOLIPID MEMBRANE => EICOSANOID SYNTHESIS
OXYGENATED BY CYCLOOXYGENASE, LIPOOXYGENASE, OR CYTOCHROME P450 TO => EICOSANOID PRODUCT
MOST IMPORTANT PRODUCT = PROSTANOIDS - MAINTAIN KEY ROLES IN PAIN SENSING

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10
Q

PROSTANOIDS

A

PRODUCED BY OXYGENATION BY 2 ENZYMES - COX-1 AND COX-2
1.) POSTAGLANDIN
2.) PROSTACYCLIN
3.) THROMBOXANE (KEY ROLE IN BLOOD CLOTTING)
ALL ARE LOCALLY PRODUCED FOR IMMEDIATE ACTION

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11
Q

COX-1

A

CONTINUOUSLY MADE AND AVAILABLE TO THE BODY 24/7
PROMOTES CLOTTING, PROTECTS GI MUCOSA, MAINTAINS KINDEY VASODILATION
I.E. ALL REGULAR PHYSIOLOGICAL FUNCTIONS

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12
Q

COX-2

A

INDUCIBLE BY VARIOUS INSULTS AND PRODUCTS INVOLVED IN INFLAMMATION/CANCER
COX-2 INHIBITORS CAN BE TAKEN FOR ARTHRITIS
ACTIVATED BY LOCAL INFLAMMATION, MODULATE PAIN, PERCEPTION AND PROMOTES FEVER

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13
Q

NSAIDS / ASPIRIN

A

NON-STEROIDAL ANTI-INFLAMMATORY DRUGS
BLOCK ENZYMES (SELECTIVELY, NON-SELECTIVELY, REVERSIBLY, IRREVERSIBLY)
INVOLVED IN SYNTHESIS OF PROSTAGLANDIN-2 CYCLOOXYGENASE AND PROSTANOID

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14
Q

MECHANISM OF ACTION OF NSAIDS/ASPIRIN

A

DECREASED VASODILATION BY PRG-2 WHICH MEANS LESS VASODILATION AND LESS EDEMA
LESS SENSITIZATION OF NOCICEPTIVE NERVE ENDINGS TO BK/5-HT MEDIATORS (IF NO PRG-2 PRODUCED THEN CAN’T RESPOND TO BK/5-HT STIMULUS)
ANTIPYRETIC - DUE TO DECREASE IN PRG-2 RESPONSE TO IL-1
ANTIPLATELET - (IR)REVERSIBLE (ASPIRIN) INHIBITION OF THROMBOXANE SYNTHESIS ; HOWEVER’ WHERE OTHER TISSUES CAN JUST MAKE MORE THROMBOXANE, PLATELETS AREN’T CELLS AND TAKE A LONG TIME TO MAKE MORE THROMBOXANE

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15
Q

ADVERSE EFFECTS OF COX-1 INHIBITION

A

GASTRIC ULCERS
BLEEDING
ACUTE RENAL FAILURE
DUE TO FAILURE TO MAKE PRG

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16
Q

ADVERSE EFFECTS OF COX-2 INHIBITION

A

REDUCES INFLAMMATION
REDUCES PAIN
REDUCES FEVER
INHIBITION OF COX => DECREASED ABILITY OF BLOOD TO CLOT (MI RISK)

17
Q

NSAID SELECTIVITY FOR COX-1/2

A

VARIED SELECTIVITY
WIDE RANGE OF DURATION 1-60HRS
MANY ARE SELECTIVELY IN THE MIDDLE

18
Q

PHARMACOKINETICS OF ASPIRIN

A

ABSORPTION - STOMACH/INTESTINES
DISTRIBUTION - READILY, INTO MOST FLUIDS/TISSUES
METABOLISM - HEPATIC
CONTRAINDICATED USES - FEVERISH CHILDREN (CAUSES REYE’S SYNDROME OF LIVER DEGENERATION AND ENCEPHALITIS IF TREATED W/ ASPIRIN DURING A VIRAL INFECTION RELATED TO VARICELLA/INFLUENZA)
**FATAL OVERDOSE IS COMMON IN CHILDREN

19
Q

ACETOMINOPHEN (APAP)

A

ANALGESIC AND ANTIPYRETIC
NOT AN NSAID BUT HAS SIMILAR EFFECTS
INHIBITS PRG-2 SYNTHESIS VIA CNS INHIBITION OF COX (NOT PERIPHERAL)
DOES NOT PROMOTE ULCERS, BLEEDING, OR RENAL FAILURE
PERIPHERALLY BLOCKS GENERATION OF PAIN IMPULSES AND INHIBITS HYPOTHALAMIC HEAT REGULATION
LIVER METABOLISM

20
Q

LIVER METABOLISM OF APAP

A

MAJOR PATHWAY - PRODUCES A NON TOXIC METABOLITE
MINOR PATHWAY - PRODUCES A HIGHLY REACTIVE INTERMEDIATE AT TOXIC APAP LEVELS
CAN NOT KEEP UP WITH METABOLISM OF APAP AND INCREASES CONCENTRATION OF REACTIVE INTERMEDIATE => HEPATIC TOXICITY AND NECROSIS
ALCOHOL CONSUMPTION CAN ALSO CAUSE THIS
PHARMACOKINETICS OF APAP - ACETYLCYSTEINE FOR OVERDOSE

21
Q

POTENTIAL TOXICITIES OF NSAIDS DUE TO PROSTANOID INHIBITION

A
  1. ) GASTRIC MUCOSAL DAMAGE, ULCERS, BLEEDING OBSTRUCTION - DUE TO PGE INHIBITION
  2. ) BLEEDING - INHIBITION OF PLATELET AGGREGATION
  3. ) LIMITATION OF RENAL BLOOD FLOW - NA+ AND WATER RETENTION, ACUTE, RENAL FAILURE, HYPERKALEMIA, HYPERTENSION
  4. ) DELAY/PROLONGATION OF LABOR
  5. ) ASTHMA AND ANAPHYLACTOID REACTIONS